- HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
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The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.
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Paragraph 0400
(2014/05/20)
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- Scalable synthesis of 4-substituted 5-bromo-6-methylpyrimidines
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Small halogenated heteroaromatic ring systems are valuable monomers, which can enable rapid access to novel and desirable chemical space, in part because of their ability to participate in established cross coupling chemistry such as the Heck, Stille, and Suzuki reactions. Described is a practical, scalable synthetic route towards the construction of a diverse array of 4-substituted 5-bromo-6-methylpyrimidine monomers. Georg Thieme Verlag Stuttgart · New York.
- Wang, Zhihan,Chi, Yushi,Harris, Anthony R.,Gray, David,Davoren, Jennifer E.
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experimental part
p. 1529 - 1531
(2011/06/23)
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- Studies on Pyrimidine Derivatives. XXXIX. Site-Selectivity in the Reaction of 5-Substituted and 4,5-Disubstituted Pyrimidine N-Oxides with Trimethylsilyl Cynanide
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The site-selectivity in the modified Reissert-Henze reaction of 5-substituted and 4,5-disubstituted pyrimidine 1-oxides with trimethylsilyl cyanide was examined.The reaction of 5-substituted 4-methoxypyrimidine 1-oxides with trimethylsilyl cyanide gave exclusively 2-pyrimidinecarbonitriles in good yields without exception.On the other hand, the other 5-substituted and 4,5-disubstituted pyrimidine 1-oxides gave mainly 6-pyrimidinecarbonitriles.Keywords--site-selectivity; pyrimidine N-oxide; trimethylsilyl cyanide; Reissert-Henze reasction; pyrimidinecarbonitrile
- Yamanaka, Hiroshi,Sakamoto, Takao,Nishimura, Sumiko,Sagi, Mataichi
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p. 3119 - 3126
(2007/10/02)
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